PS-1145 二盐酸盐

C₁₇H₁₁ClN₄O · 2HCl

395.67

MFCD08705411

24724584

NA.77

PS-1145 dihydrochloride has been used as an IκB kinase (IKK) inhibitor:

• in the culture medium to treat human epidermal keratinocytes (HEKs) and squamous carcinoma cells (SCCs) to study the role of IKK in Corynebacterium tuberculostearicum (C. t.)-elicited transcription of inflammatory mediators
• to investigate the involvement of transcription factor p65 (RelA)/nuclear factor kappa-B (NF-κB) in the cluster of differentiation 28 (CD28)-mediated interleukin-17A (IL-17A) gene expression
• to examine the involvement of NF-κB signaling in the cytotoxic effect of niclosamide on colorectal cancer (CRC) cells

PS-1145, a β-carboline derivative, blocks the phosphorylation and degradation of the inhibitor of nuclear factor kappa-β (NF-κB;). It also inhibits the subsequent activation of nuclear factor kappa-β (NF-κB) and thereby prevents the release of tumor necrosis factor-α (TNF-α) in lipopolysaccharide treated mice. PS-1145 hinders pro-inflammatory cytokine production and cell proliferation. It plays a potential therapeutic role in carcinogenesis in multiple myeloma. PS-1145 exhibits anti-tumor activity on nasopharyngeal carcinoma (NPC) cell lines.
PS-1145 is an IKB kinase (IKK) inhibitor.

This compound is featured on the MAPKKKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

100

≥98% (HPLC)

solid

yellow

DMSO: >3 mg/mL at ~60 ℃, clear (with warming for 2 minutes)
methanol: water (1:1): ≥5 mg/mL at 60 ℃ (With warming for 5 minutes.)

2-8℃

Cl[H].Cl[H].Clc1cc(NC(=O)c2cccnc2)c3[nH]c4cnccc4c3c1

1S/C17H11ClN4O.2ClH/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10;;/h1-9,21H,(H,22,23);2*1H

QTDCBADLGJZBHP-UHFFFAOYSA-N

5, 25 mg in glass bottle

GHS07

Warning

H302

Acute Tox. 4 Oral

11 - Combustible Solids

WGK 3

dust mask type N95 (US), Eyeshields, Gloves